期刊
JOURNAL OF CONTROLLED RELEASE
卷 75, 期 3, 页码 365-379出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/S0168-3659(01)00405-9
关键词
N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer; anticancer drug; camptothecin; colon-specific drug delivery; drug release
资金
- FIC NIH HHS [TW00991] Funding Source: Medline
- NIDDK NIH HHS [DK39544] Funding Source: Medline
N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer conjugates for colon-specific delivery of 9-aminocamptothecin (9-AC) were designed. They hold 9-AC bound via spacers containing amino acid residues and aromatic azo bonds. In vitro release profiles of 9-AC from HPMA copolymer conjugates were evaluated under artificial conditions that simulated large intestinal azoreductase and peptidase activities. The studies indicated that the azo bond was reduced first, followed by the release of unmodified 9-AC from the 9-AC containing fragment by peptidases. Release profiles depended on the chemical structure of the peptide part of the spacer. Conjugates containing leucylalanine showed high colon-specific release of 9-AC when compared to alanine containing conjugates. It appears that the studied conjugates are suitable as colon-specific drug delivery systems. (C) 2001 Elsevier Science BY All rights reserved.
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